MG-262 (also known as Z-Leu-Leu-Leu-B(OH)2), a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome. It consists of a peptide and boronic acid moiety which are functional to proteasome inhibition. According to previous studies, MG-262 is capable of reducing the viability of nasal mucosa and polyp fibroblasts, provoking cell growth arrest, inhibiting DNA replication and retinoblastoma phosphorylation, increasing expression of the cell cycle inhibitor p21 and p27, and inducing cell death via loss of mitochondrial membrane potential, caspase-3 and poly(ADP-ribose) polymerase activation, induction of c-Jun phosphorylation and mitogen-activated protein kinase phosphatase-1 expression. .Laura Pujols, Laura Fernandez-Bertolin, Mireya Fuentes-Prado, Isam Alobid, Jordi Roca-Ferrer, Neus Agell, Joaquim Mullol, and Cesar Picado. Proteasome inhibition reduces proliferation, collagen expression, and inflammatory cytokine production in nasal mucosa and polyp fibroblasts. The Journal of Pharmacology and Experimental Therapeutics 2012; 343:184-197 .Hilary Frase, Jason Hudak, and Irene Lee. Identification of the proteasome inhibitor MG262 as a potent ATP-dependent inhibitor of the Salmonella enteric serovar typhimurium lon protease. Biochemistry 2006; 45 (27): 8264-8274

Product information

CAS Number: 179324-22-2

Molecular Weight: 491.43

Formula: C25H42BN3O6

Chemical Name: {1-[2-(2-{[(benzyloxy)carbonyl]amino}-4-methylpentanamido)-4-methylpentanamido]-3-methylbutyl}boronic acid

Smiles: CC(C)CC(NC(=O)OCC1C=CC=CC=1)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)B(O)O

InChiKey: MWKOOGAFELWOCD-UHFFFAOYSA-N

InChi: InChI=1S/C25H42BN3O6/c1-16(2)12-20(24(31)29-22(26(33)34)14-18(5)6)27-23(30)21(13-17(3)4)28-25(32)35-15-19-10-8-7-9-11-19/h7-11,16-18,20-22,33-34H,12-15H2,1-6H3,(H,27,30)(H,28,32)(H,29,31)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.